Kudlacz E M
Pfizer Central Research Division, Groton, CT 06340, USA.
Expert Opin Investig Drugs. 1998 Jul;7(7):1055-62. doi: 10.1517/13543784.7.7.1055.
The tachykinins, substance P (SP) and neurokinin A (NK-A), are thought to be key players in the process of neurogenic inflammation, which is believed to contribute to the pathogenesis of various respiratory diseases. Due to the additive nature of the respiratory effects of these sensory neuropeptides, inhibiting the effects of tachykinins at both NK1 and NK2 receptors may represent a therapeutic advantage for the treatment of asthma, as opposed to receptor-selective antagonists, which have demonstrated only minimal efficacy to date. A number of companies are pursuing small molecule approaches yielding compounds with potent, balanced NK1 and NK2 receptor antagonist activities. In allergic rhinitis, NK1 receptor antagonism may complement the actions of antihistamines by addressing nasal congestion, which is largely unrelieved by these otherwise highly efficacious agents. Novel combined H1/NK1 receptor antagonists have been developed and may represent a therapeutic option for the treatment of this disease.
速激肽、P物质（SP）和神经激肽A（NK - A）被认为是神经源性炎症过程中的关键参与者，而神经源性炎症被认为与多种呼吸系统疾病的发病机制有关。由于这些感觉神经肽对呼吸的作用具有累加性，与迄今仅显示出极小疗效的受体选择性拮抗剂相比，抑制速激肽在NK1和NK2受体上的作用可能对哮喘治疗具有治疗优势。许多公司正在采用小分子方法来生产具有强效、平衡的NK1和NK2受体拮抗活性的化合物。在过敏性鼻炎中，NK1受体拮抗作用可能通过解决鼻充血来补充抗组胺药的作用，而鼻充血在很大程度上不能被这些原本高效的药物缓解。新型H1/NK1受体联合拮抗剂已被开发出来，可能代表了治疗这种疾病的一种治疗选择。
